2. Academic Validation
  3. Introduction of new quinolone-2-thio-acetamide-propane hydrazide-benzimidazole derivatives as new α-glucosidase and α-amylase inhibitors

Introduction of new quinolone-2-thio-acetamide-propane hydrazide-benzimidazole derivatives as new α-glucosidase and α-amylase inhibitors

  • Sci Rep. 2025 Aug 26;15(1):31349. doi: 10.1038/s41598-025-16661-7.
Parisa Nikfar 1,  Somaye Karimian 2,  Sajedeh Safapoor 3,  Milad Noori 3,  Navid Dastyafteh 3,  Seyedeh Niloufar Ghafouri 4,  Maryam Mohammadi-Khanaposhtani 5,  Bagher Larijani 3,  Parham Taslimi 6,  Mohammad Mahdavi 7
Affiliations

Affiliations

  • 1 Department of Medicinal Chemistry, School of Pharmacy, Iran University of Medical Sciences, Tehran, Iran.
  • 2 Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran.
  • 3 Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran.
  • 4 School of Chemistry, College of Science, University of Tehran, Tehran, Iran.
  • 5 Cellular and Molecular Biology Research Center, Health Research Institute, Babol University of Medical Sciences, Babol, Iran.
  • 6 Department of Biotechnology, Faculty of Science, Bartin University, Bartin, Türkiye. parham_taslimi_un@yahoo.com.
  • 7 Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran. momahdavi@tums.ac.ir.
PMID: 40858721 DOI: 10.1038/s41598-025-16661-7
Abstract

In the present work, new quinolone-2-thio-acetamide-propane hydrazide-benzimidazole derivatives 12a-o were assigned as potent anti-diabetic agents that targeting α-glucosidase and α-amylase as two important targets in treatment of type 2 diabetes. General scaffold of these compounds was designed based on the reported potent α-glucosidase and α-amylase inhibitors and derivation was performed in acetamide moiety. In vitro evaluation of the new compounds 12a-o demonstrated that most of the synthesized compounds were more potent than standard inhibitor acarbose against α-glucosidase while all these new compounds were more potent than acaerbose against α-amylase. The most potent compound against both studied Enzymes was compound 12n that was a 4-fluorophenylacetamide derivative. This compound was 5 and 23.8 folds more potent than acarbose against α-glucosidase and α-amylase, respectively, and with excellent binding energies in comparison to acarbose attached to active sites of these Enzymes. Molecular dynamics and pharmacokinetic studies of compound 12n was also performed.

Keywords

Benzimidazole; Propane hydrazide; Quinolone-2-thio-acetamide; Α-Amylase; Α-Glucosidase.

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